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Article

Construction and Biological Evaluation of a Novel Integrin ανβ3-Specific Carrier for Targeted siRNA Delivery In Vitro

Department of Nuclear Medicine, Peking University First Hospital, No. 8, Xishiku St., West District, Beijing 100034, China
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Authors to whom correspondence should be addressed.
Academic Editor: Harri Lönnberg
Molecules 2017, 22(2), 231; https://doi.org/10.3390/molecules22020231
Received: 31 December 2016 / Revised: 28 January 2017 / Accepted: 1 February 2017 / Published: 4 February 2017
(This article belongs to the Special Issue Synthesis and Applications of Oligonucleotide Conjugates)
(1) Background: The great potential of RNA interference (RNAi)-based gene therapy is premised on the effective delivery of small interfering RNAs (siRNAs) to target tissues and cells. Hence, we aimed at developing and examining a novel integrin αvβ3-specific delivery carrier for targeted transfection of siRNA to malignant tumor cells; (2) Methods: Arginine-glycine-aspartate motif (RGD) was adopted as a tissue target for specific recognition of integrin αvβ3. To enable siRNA binding, a chimeric peptide was synthesized by adding nonamer arginine residues (9R) at the carboxy terminus of cyclic-RGD dimer, designated as c(RGD)2-9R. The efficiency of 9R peptide transferring siRNA was biologically evaluated in vitro by flow cytometry, confocal microscopy, and Western blot; (3) Results: An optimal 10:1 molar ratio of c(RGD)2-9R to siRNA was confirmed by the electrophoresis on agarose gels. Both the flow cytometry and confocal microscopy results testified that transfection of c(RGD)2-9R as an siRNA delivery carrier was obviously higher than the naked-siRNA group. The results of Western blot demonstrated that these 9R peptides were able to transduce siRNA to HepG2 cells in vitro, resulting in efficient gene silencing; and (4) Conclusion: The chimeric peptide of c(RGD)2-9R can be developed as an effective siRNA delivery carrier and shows potential as a new strategy for RNAi-based gene therapy. View Full-Text
Keywords: RNA interference (RNAi); small interfering RNA (siRNA); arginine-glycine-aspartate (RGD); integrin αvβ3 RNA interference (RNAi); small interfering RNA (siRNA); arginine-glycine-aspartate (RGD); integrin αvβ3
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MDPI and ACS Style

Chen, X.; Liu, M.; Wang, R.; Yan, P.; Zhang, C.; Ma, C.; Yin, L. Construction and Biological Evaluation of a Novel Integrin ανβ3-Specific Carrier for Targeted siRNA Delivery In Vitro. Molecules 2017, 22, 231. https://doi.org/10.3390/molecules22020231

AMA Style

Chen X, Liu M, Wang R, Yan P, Zhang C, Ma C, Yin L. Construction and Biological Evaluation of a Novel Integrin ανβ3-Specific Carrier for Targeted siRNA Delivery In Vitro. Molecules. 2017; 22(2):231. https://doi.org/10.3390/molecules22020231

Chicago/Turabian Style

Chen, Xueqi, Meng Liu, Rongfu Wang, Ping Yan, Chunli Zhang, Chao Ma, and Lei Yin. 2017. "Construction and Biological Evaluation of a Novel Integrin ανβ3-Specific Carrier for Targeted siRNA Delivery In Vitro" Molecules 22, no. 2: 231. https://doi.org/10.3390/molecules22020231

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